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    • 3. 发明申请
    • ACID AMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    • 酰胺衍生物及其制备方法
    • WO1995031443A1
    • 1995-11-23
    • PCT/HU1995000015
    • 1995-05-18
    • EGIS GYOGYSZERGYAR RT.RIVO, EndreVIZI, E., SzilveszterMAKARA, GáborREITER, JózsefBLASKO, GáborSIMIG, GyulaGAAL, LászlóFEKETE, Márton
    • EGIS GYOGYSZERGYAR RT.
    • C07D241/44
    • C07D241/44
    • The invention relates to new acid amide derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said acid amide derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The new compounds according to the invention can be characterized by formula (I), wherein R represents hydrogen or nitro, R and R stand, independently from each other, for hydrogen, lower alkyl or lower alkenyl optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated heteroring containing 1 or 2 nitrogen and/or oxygen atom(s); or R and R form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group containing optionally 1 or 2 additional nitrogen atoms and/or oxygen atom(s), said ring optionally carrying a hydroxy or a hydroxy-lower alkyl group, and possess valuable AMPA and kainate antagonizing properties, so they can be used to advantage in the therapy.
    • 本发明涉及新的酰胺酰胺衍生物,其制备方法,包含该酰胺衍生物的药物组合物,涉及使用所述酰胺酰胺衍生物用于治疗疾病和用于制备适于治疗疾病的药物组合物。 根据本发明的新化合物可以通过式(I)表征,其中R 1表示氢或硝基,R 2和R 3彼此独立地表示氢,低级烷基或低级烯基 任选地带有选自卤素,羟基,低级烷氧基,二(低级烷基)氨基,苯基 - 低级烷氧基羰基和含有1或2个氮和/或氧原子的5-至6-元饱和杂环的取代基 ); 或R 2和R 3与相邻的氮原子一起形成含有任选1或2个另外的氮原子和/或氧原子的6元饱和杂环基,所述环任选地带有羟基或 羟基低级烷基,具有有价值的AMPA和红藻氨酸盐拮抗性,因此可用于治疗。